A set of 1-(arylalkyl)quinolizidines, isosteric thio analogs, and variously functionalized congeners were synthesized and tested for affinity to sigma1 and sigma2 receptor subtypes, by displacing [3H]-(+)-pentazocine and [3H]DTG from guinea pig brain and rat brain prepns., resp. All compds. exhibited a good affinity for the sigma1 subtype, with subnanomolar Ki values for the best of them, while only modest or poor affinity for the sigma2 subtype was obsd. Some structure-activity relationships were put forward.
1-(arylalkyl)quinolizidine derivatives and thio-isosteric analogs as ligands for sigma receptors / A. Sparatore, F. Novelli, F. Sparatore. - In: HELVETICA CHIMICA ACTA. - ISSN 0018-019X. - 87:3(2004), pp. 580-591. [10.1002/hlca.200490055]
1-(arylalkyl)quinolizidine derivatives and thio-isosteric analogs as ligands for sigma receptors
A. Sparatore
;
2004
Abstract
A set of 1-(arylalkyl)quinolizidines, isosteric thio analogs, and variously functionalized congeners were synthesized and tested for affinity to sigma1 and sigma2 receptor subtypes, by displacing [3H]-(+)-pentazocine and [3H]DTG from guinea pig brain and rat brain prepns., resp. All compds. exhibited a good affinity for the sigma1 subtype, with subnanomolar Ki values for the best of them, while only modest or poor affinity for the sigma2 subtype was obsd. Some structure-activity relationships were put forward.
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